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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC74750 Kanamycin A sulfate Kanamycin, also known as kanamycin A, is an aminoglycoside bacteriocidal antibiotic, available in by mouth, intravenous, and intramuscular forms, and used to treat a wide variety of infections. Kanamycin is isolated from the bacterium Streptomyces kanamyceticus and its most commonly used form is kanamycin sulfate. Kanamycin interacts with the 30S subunit of prokaryotic ribosomes. It gives birth to substantial amounts of mistranslation and indirectly inhibits translocation during protein synthesis.
DC74751 SAR407899 free base SAR407899 is a potent and selective Rho kinase inhibitor with promising antihypertensive activity. SAR407899 potently inhibits endothelin-1-induced constriction of renal resistance arteries. SAR407899 is equipotent against human and rat-derived Rho-kinase 2 with inhibition constant values of 36 nM and 41 nM, respectively. SAR407899 is approximately 8-fold more active than fasudil. SAR407899 potently (mean IC(50) values: 122 to 280 nM) and species-independently relaxed precontracted isolated arteries of different species and different vascular beds. The antihypertensive effect of SAR407899 was superior to that of fasudil and Y-27632.
DC74752 SARS-CoV-2-IN-39 SARS-CoV-2-IN-39 (compound 21) is a SARS-CoV-2 inhibitor with an EC50 of 1 μM.
DC74753 L-Tyrosinol HCl L-Tyrosine is an aromatic, polar, non-essential amino acid that contains a highly reactive α-amino, α-carboxyl, and phenolic hydroxyl group. L-tyrosine modulates biofilm formation of Bacillus cereus ATCC 14579. L-Tyrosine Limits Mycobacterial Survival in Tuberculous Granuloma.
DC74754 SB-277011 HCl SB-277011, also known as SB-277011-A, is an orally active, potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat. SB-277011 potentiated phMRI response to acute amphetamine challenge in the rat brain. SB-277011 attenuated ethanol consumption in ethanol preferring (P) and non-preferring (NP) rats.
DC74755 Prulifloxacin Prulifloxacin, also known as NM-441, is an inhibitor of bacterial DNA gyrase used to treat urinary tract infections. Prulifloxacin is an oral fluoroquinolone with a broad in vitro activity spectrum against Gram positive and negative bacteria and among fluoroquinolones has the lowest power of inducing resistance. In vitro and in vivo studies have shown its clinical efficacy and pathogen eradication.
DC74756 (-)-GSK598809 HCl (-)-GSK598809 is an isomer of GSK598809. GSK598809 is a selective D(3)R antagonist recently progressed in Phase I trials. GSK-598809 may decrease the rewarding effects of contextual cues associated with drug intake preclinically, which may reduce drug craving in humans.
DC74757 Tirabrutinib free base Tirabrutinib, also known as ONO-4059 and GS-4059, is a potent and orally active Bruton agammaglobulinemia tyrosine kinase (BTK) in hibitor. Upon administration, ONO-4059 covalently binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. As a result, this agent may inhibit the proliferation of B-cell malignancies. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.
DC74758 Rupatadine Fumarate Rupatadine Fumarate, also known as Rupatadine, is a second-generation H1-antihistamine with dual affinity for histamine H1 and PAF receptors. Rupatadine is indicated for the treatment of allergic rhinitis and urticaria.
DC74759 GSK-1034702 GSK-1034702 is a potent M1 receptor allosteric agonist. GSK-1034702, a selective M(1) receptor allosteric agonist, may have therapeutic benefits in disorders of impaired learning including Alzheimer's disease.
DC74760 Sonidegib phosphate Sonidegib (also known as erismodegib, LDE225, and NVP-LDE225) is an orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity. Erismodegib selectively binds to the Hedgehog (Hh)-ligand cell surface receptor Smo, which may result in the suppression of the Hh signaling pathway and, so, the inhibition of tumor cells in which this pathway is abnormally activated. It was approved by the FDA for treating basal cell carcinoma in July 2015.
DC74761 MPEP HCl MPEP is a selective mGluR5 antagonist. MPEP reverses maze learning and PSD-95 deficits in Fmr1 knock-out mice. MPEP elevates accumbal dopamine and glycine levels; interaction with strychnine-sensitive glycine receptors. MPEP activates specific stress-related brain regions and lacks neurotoxic effects of the NMDA receptor antagonist MK-801: significance for the use as anxiolytic/antidepressant drug.
DC74762 S1R agonist 2 S1R agonist 2 (Compound 8b) is a selective S1R agonist.
DC74763 CpCDPK1/TgCDPK1-IN-3 CpCDPK1/TgCDPK1-IN-3 (Compound 20) is a CpCDPK1 and TgCDPK1 inhibitor
DC74764 DOTMA E-isomer DOTMA E-isomer is a trans-isomer of DOTMA, in which two double bonds are trans-configuration (configuration of a geometrical isomer in which two groups are on opposite sides of an imaginary reference line on the molecule). DOTMA E-isomer is a useful cationic lipid for gene transfection, nucleic acids delivery, plasmid stabilization. Note: DOTMA is the Z-isomer (or Cis-isomer) chloride salt, which CAS# is 104162-48-3. While DOTMA E-isomer (trans-isomer) chloride salt has CAS#104872-42-6. Some vendors confused each other.
DC74765 Manidipine HCl Manidipine, also known as CV-4093, is a calcium channel blocker (dihydropyridine type) that is used clinically as an antihypertensive. Manidipine is a lipophilic, third-generation dihydropyridine calcium channel antagonist with a high degree of selectivity for the vasculature, thereby inducing marked peripheral vasodilation with negligible cardiodepression. In addition, manidipine does not significantly affect norepinephrine levels, suggesting a lack of sympathetic activation. Manidipine has shown antihypertensive efficacy and appears to be well tolerated in adult and elderly patients with mild or moderate essential hypertension.
DC74766 ARTD3/PARP3-IN-1 ARTD3/PARP3-IN-1 is an unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3)/PARP3.
DC74767 NDM-1 inhibitor-3 NDM-1 inhibitor-3 (Compound 89) is a New Delhi Metallo-β-lactamase-1 (NDM-1) inhibitor
DC74768 Tosufloxacin tosylate Tosufloxacin, also known as T-3262, is a fluoroquinolone antibiotic used to treat susceptible infections. It has a controversial safety profile in relation to other fluoroquinolones. It is associated with severe thrombocytopenia and nephritis, and hepatotoxicity. It is sold in Japan under the brand name Ozex.
DC74769 NSC-87877 free acid NSC-87877 is a cell-permeable, inhibitor of both SHP-1 and SHP-2 (IC50 = 355 and 318 nM, respectively). NSC-87877 shows effective growth inhibition and induction of apoptosis in NB cell lines. In an intrarenal mouse model of NB, NSC-87877 treatment results in decreased tumor growth and increased p53 and p38 activity. DUSP26 inhibition with NSC-87877 is an effective strategy to induce NB cell cytotoxicity in vitro and in vivo through activation of the p53 and p38 mitogen-activated protein kinase (MAPK) tumor-suppressor pathways.
DC74770 Tubulin inhibitor 32 Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor.
DC74771 Ulipristal acetate Ulipristal acetate, also known as CDB-2914, is a selective progesterone receptor modulator (SPRM) approved for contraception, and for uterine fibroid. As a SPRM, ulipristal acetate has partial agonistic as well as antagonistic effects on the progesterone receptor. It also binds to the glucocorticoid receptor, but is only a weak antiglucocorticoid relative to mifepristone, and has no relevant affinity to the estrogen, androgen and mineralocorticoid receptors.
DC74772 SLx-2119 SLx-2119, also known as KD-025 and Belumosudil, is an orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 µM, respectively).
DC74773 VU0364572 free base VU0364572 free base is an orally active and selective allosteric agonist of the M1 muscarinic receptor.
DC74774 SHP099 HCl SHP099 is a potent, selective, orally bioavailable, and efficacious SHP2 inhibitor with IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM. SHP099 exhibits dose-dependent pathway inhibition and antitumor activity in xenograft models. SHP2 is a nonreceptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene involved in cell growth and differentiation via the MAPK signaling pathway. SHP2 also purportedly plays an important role in the programmed cell death pathway (PD-1/PD-L1). Because it is an oncoprotein associated with multiple cancer-related diseases, as well as a potential immunomodulator, controlling SHP2 activity is of significant therapeutic interest.
DC74775 VU0364572 TFA VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor.
DC74776 HT-61 HT-61, also known as HY-50A, is a pyrroloquinolone antibiotic potentially for the treatment of staphylococcal infections. HT61 was effective at reducing biofilm viability and was associated with increased expression of cell wall stress and division proteins, confirming its potential as a treatment for S. aureus biofilm infections. HT61 enhances the effect of tobramycin against Pseudomonas aeruginosa in vitro and in vivo.
DC74777 Ivermectin Ivermectin is a medication that is effective against many types of parasites. It is used to treat head lice, scabies, river blindness, strongyloidiasis, and lymphatic filariasis, among others. Ivermectin and other avermectins (insecticides most frequently used in home-use ant baits) are macrocyclic lactones derived from the bacterium Streptomyces avermitilis. Ivermectin kills by interfering with nervous system and muscle function, in particular by enhancing inhibitory neurotransmission. Ivermectin is a mixture of mostly avermectin H2B1a (CAS# 71827-03-7) with some avermectin H2B1b (CAS# 70209-81-3), which are macrolides from STREPTOMYCES avermitilis.
DC74778 LY 43578 LY 43578 is an aromatase inhibitor.
DC74779 TASK-1-IN-1 TASK-1-IN-1 is a potent and selective TASK-1 inhibitor.

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